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Injection containing triamcinolone acetonide and PLGA sustained release microspheres, preparation method of injection and application of injection to preparation of medicine for treating osteoarthritis pain

A technology of slow-release microspheres and injections, applied in drug combination, drug delivery, antipyretics, etc., can solve the problems of patient burden, achieve the effects of reducing patient burden, prolonging analgesic time, and reducing the number of injections

Inactive Publication Date: 2017-07-28
江苏富泽药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Traditional immediate-release triamcinolone acetonide injections require frequent intra-articular injections in the treatment of osteoarthritis pain, which poses a great burden on patients, and the drug effect lasts for about two weeks after single administration

Method used

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  • Injection containing triamcinolone acetonide and PLGA sustained release microspheres, preparation method of injection and application of injection to preparation of medicine for treating osteoarthritis pain
  • Injection containing triamcinolone acetonide and PLGA sustained release microspheres, preparation method of injection and application of injection to preparation of medicine for treating osteoarthritis pain
  • Injection containing triamcinolone acetonide and PLGA sustained release microspheres, preparation method of injection and application of injection to preparation of medicine for treating osteoarthritis pain

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Embodiment 1

[0025] 1. Preparation of drug-loaded sustained-release microspheres

[0026] Composite PLGA sustained-release microspheres loaded with triamcinolone acetonide were prepared by solvent evaporation method. Proceed as follows:

[0027] Accurately weigh 50 mg of PLGA, dissolve it in 1 ml of dichloromethane, add 7.5 mg of triamcinolone acetonide, and hyaluronic acid freeze-induced layered vitrified particles (containing 5 mg of hyaluronic acid), vortex to fully dissolve, and form an organic phase. Draw the organic phase with a 1ml syringe, slowly inject it into 50ml of 3% PVA aqueous solution, stir with electric force at 1000rpm for 3 minutes, and continue magnetic stirring for 5 hours. The solidified drug-loaded microspheres were suction-filtered through a 0.22 μm microporous membrane, washed repeatedly with 500 ml of distilled water, collected the drug-loaded microspheres, and vacuum freeze-dried to obtain triamcinolone-loaded composite PLGA microspheres.

[0028] The experimen...

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Abstract

The invention provides injection containing triamcinolone acetonide and PLGA sustained release microspheres, a preparation method of the injection and application of the injection to the preparation of medicine for treating osteoarthritis pain. The injection comprises the triamcinolone acetonide, PLGA copolymer and hyaluronic acid, wherein the weight ratio of the PLGA to the triamcinolone acetonide is 100:(5-25); the weight ratio of the PLGA to the hyaluronic acid is 100:(5-15). The injection has the advantages that the medicine-loading sustained release microspheres are good in stability; the PLGA microspheres are used to wrap the triamcinolone acetonide, the medicine can be released in a sustained manner, medicine stability can be increased, and medicine hydrolysis can be reduced; the detection result of a reverse-phase hydrophobic high-performance liquid phase method shows that the quick release triamcinolone acetonide released in an aqueous solution in an in-vitro manner has evident degradation and absorption peaks and the triamcinolone acetonide wrapped in the microspheres is complete in structure and does not have evident degradation and absorption peaks; the hyaluronic acid has a synergistic effect, and due to the fact that hyaluronic acid improves knee joint viscosity, the clearance rate of the triamcinolone acetonide is further reduced, and acting time is prolonged.

Description

technical field [0001] The present invention relates to a sustained-release injection preparation for osteoarthritis pain treatment, specifically, the present invention is to prepare a sustained-release preparation containing triamcinolone acetonide, which slowly releases the drug triamcinolone acetonide through intra-articular injection, and at the same time Hyaluronic acid is compounded in the sustained-release microspheres, which increases the efficacy of the preparation, thereby achieving the effect of long-term control of osteoarthritis pain, reducing the frequency of injections, and increasing patient compliance. The preparation process is simple and the side effects of the sustained-release injection are low. A new formulation with great clinical application. Background technique [0002] Mediators in inflammation can activate or sensitize pain-sensing nerves (nociceptors), which in normal joints respond only to severe stress and extreme motion beyond the joint's norm...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K31/58A61K47/34A61K47/36A61P19/02A61P19/08A61P29/00
CPCA61K9/5031A61K9/0002A61K9/0019A61K31/58A61K47/36
Inventor 何智健谢卫锋吴鹏程李浩源
Owner 江苏富泽药业有限公司
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